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J Med Chem. 2015 Jul 23;58(14):5684-8. doi: 10.1021/acs.jmedchem.5b00498. Epub 2015 Jul 6.

Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase γ.

Author information

1
Vertex Pharmaceuticals Inc., 50 Northern Avenue, Boston, Massachusetts 02210, United States.

Abstract

A series of high affinity second-generation thiazolopiperidine inhibitors of PI3Kγ were designed based on some general observations around lipid kinase structure. Optimization of the alkylimidazole group led to inhibitors with higher levels of PI3Kγ selectivity. Additional insights into PI3K isoform selectivity related to sequence differences in a known distal hydrophobic pocket are also described.

PMID:
26121481
DOI:
10.1021/acs.jmedchem.5b00498
[Indexed for MEDLINE]

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